ML 2-23
ML 2-23 is a PROTAC degrader that recruits RNF114 to target BCR-ABL/c-ABL for degradation. ML 2-23 promotes proteasome-dependent degradation of the target protein and inhibits phosphorylation of downstream CRKL. At concentrations used for BCR-ABL degradation, ML 2-23 only causes slight impairment to the viability of cancer cells. ML 2-23 can be used in the research of chronic myeloid leukemia.
(Pink: Bcr-Abl Target protein ligand; Blue: RNF114 ligand (HY-28328); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C47H53BrCl2N10O7S
- 分子量:1052.86
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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BCR-ABL |
c-ABL |
ML 2-23 (0.01-5 μM; 16 h) reduces the protein levels of BCR-ABL and c-ABL in K562 cells in a concentration-dependent manner, with a stronger degradation effect on BCR-ABL than on c-ABL, while simultaneously decreasing the phosphorylation of CRKL, a downstream substrate of BCR-ABL. It only slightly reduces the viability of K562 cells in WST assays, indicating that the observed protein reduction is not caused by general cytotoxicity under the concentration and treatment time used to evaluate BCR-ABL degradation[1].
Pretreatment with ML 2-23 (1 μM; 12 h; 30 min pretreatment with 5 μM MG132 (HY-13259)) significantly reverses the ML 2-23-induced degradation of BCR-ABL and c-ABL in K562 cells, indicating that this degradation is proteasome-dependent[1].
ML 2-23 (5 μM; 16 h) does not significantly affect BCR-ABL mRNA levels in K562 cells, but increases c-ABL mRNA levels, indicating that the reduction in BCR-ABL and c-ABL proteins is not caused by transcriptional downregulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:0.01, 0.1, 0.5, 1, 5 μM
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Incubation Time:16 h
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Result:Concentration-dependently reduced BCR-ABL and c-ABL protein levels, preferentially degraded BCR-ABL over c-ABL, and decreased p-CRKL levels.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:MG132: 5 μM; 1 μM
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Incubation Time:MG132 pretreatment for 30 min; ML 2-23 treatment for 12 h
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Result:Reduced BCR-ABL and c-ABL protein levels; MG132 pretreatment significantly rescued the degradation.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:5 μM
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Incubation Time:16 h
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Result:Did not significantly alter BCR-ABL mRNA levels but increased c-ABL mRNA levels.
化学情報
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分子量 1052.86
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分子式 C47H53BrCl2N10O7S
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SMILES
O=C(COC1=CC=C(C2CC(C3=CC=C(Br)C=C3)=NN2C(CCl)=O)C=C1)NCCOCCOCCOCCN4CCN(C5=NC(C)=NC(NC6=NC=C(C(NC7=C(C)C=CC=C7Cl)=O)S6)=C5)CC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)